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Active ingredients
Ebastine
Release form
Pills
Composition
Microbial Ebastine 10 mg. Auxiliary substances: microcrystalline cellulose, corn starch, lactose monohydrate, sodium carboxymethylcellulose structured, magnesium stearate, hydroxypropylmethylcellulose, polyethylene glycol 6000, titanium dioxide.
Pharmacological effect
Antiallergic drug. After taking the drug inside the pronounced antiallergic action begins after 1 h and lasts for 48 hours. After a 5-day course of treatment with Kestine; antihistamine activity is maintained for 72 hours due to the action of active metabolites. The drug does not have a pronounced anticholinergic and sedative effect. No effect of Kestine; on a QT-interval of an ECG in the dose of 100 mg, exceeding the recommended daily dose by 5-10 times.
Pharmacokinetics
After ingestion, it is rapidly absorbed and almost completely metabolized in the liver, turning into the active metabolite carbastin. After a single dose of 10 mg of drug Cmax of carbastine in plasma is achieved in 2.6-4 hours and is 80-100 ng / ml. It does not penetrate the hemato-encephalic barrier. When daily intake of 10 mg of the drug, the equilibrium concentration is reached in 3-5 days and is 130-160 ng / ml. Plasma protein binding of ebastine and carbastine is more than 95%. T1 / 2 carbastine ranges from 15 to 19 hours, 66% of the drug is excreted in the form of conjugates through the kidneys. Food intake does not affect the clinical effects of the drug Kestine ;. In elderly patients, the pharmacokinetic parameters do not change significantly. In renal insufficiency, T1 / 2 increases to 23-26 h, and in hepatic insufficiency, to 27 h, however, the concentration of the drug does not exceed therapeutic values.
Indications
- allergic rhinitis of various etiologies (seasonal and / or year-round, both accompanied and not accompanied by allergic conjunctivitis); urticaria of various etiologies, including chronic idiopathic.
Contraindications
- hypersensitivity to the components of the drug; - pregnancy, lactation period; - children's age up to 12 years; - lactase deficiency, lactose intolerance, glucose-galactose malabsorption. or liver failure.
Precautionary measures
Use for violations of the liver, with caution in liver failure. Use for violations of the kidney function with caution for renal failure. The use in children is contraindicated in children under 12 years of age.
Use during pregnancy and lactation
Contraindicated during pregnancy and lactation.
Dosage and administration
Inside, regardless of the meal. Adults and children over 12 years old are prescribed 10-20 mg (1-2 pills) of the drug once a day. When the liver dysfunction, the daily dose should not exceed 10 mg.
Side effects
With a frequency of more than 1%: headache (7.9%), drowsiness (3.0%), dryness of the oral mucosa (2.1%). With a frequency of less than 1%: dyspepsia, nausea, insomnia, abdominal pain, asthenic syndrome, sinusitis, rhinitis.
Overdose
Signs of moderate effects on the central nervous system (fatigue) and the autonomic nervous system (dry oral mucosa) can occur only at high doses (300 mg-500 mg, which is 30-50 times higher than the therapeutic dose). There is no special antidote for Ebastine . In case of overdose, gastric lavage, monitoring of vital body functions, and symptomatic treatment are recommended.
Interaction with other drugs
Do not use the drug Kestine; simultaneously with ketoconazole and erythromycin (increased risk of prolongation of the QT interval). Kestine preparation; does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.
special instructions
Impact on the ability to drive motor vehicles and control mechanisms. In the event of side effects from the central nervous system, a minimal decrease in patients' ability to drive vehicles and engage in other potentially dangerous activities requiring increased attention span and psychomotor reactions is possible.